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Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain.
Dovey HF, John V, Anderson JP, Chen LZ, de Saint Andrieu P, Fang LY, Freedman SB, Folmer B, Goldbach E, Holsztynska EJ, Hu KL, Johnson-Wood KL, Kennedy SL, Kholodenko D, Knops JE, Latimer LH, Lee M, Liao Z, Lieberburg IM, Motter RN, Mutter LC, Nietz J, Quinn KP, Sacchi KL, Seubert PA, Shopp GM, Thorsett ED, Tung JS, Wu J, Yang S, Yin CT, Schenk DB, May PC, Altstiel LD, Bender MH, Boggs LN, Britton TC, Clemens JC, Czilli DL, Dieckman-McGinty DK, Droste JJ, Fuson KS, Gitter BD, Hyslop PA, Johnstone EM, Li WY, Little SP, Mabry TE, Miller FD, Audia JE. Dovey HF, et al. Among authors: chen lz. J Neurochem. 2001 Jan;76(1):173-81. doi: 10.1046/j.1471-4159.2001.00012.x. J Neurochem. 2001. PMID: 11145990 Free article.
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Truong AP, Tóth G, Probst GD, Sealy JM, Bowers S, Wone DW, Dressen D, Hom RK, Konradi AW, Sham HL, Wu J, Peterson BT, Ruslim L, Bova MP, Kholodenko D, Motter RN, Bard F, Santiago P, Ni H, Chian D, Soriano F, Cole T, Brigham EF, Wong K, Zmolek W, Goldbach E, Samant B, Chen L, Zhang H, Nakamura DF, Quinn KP, Yednock TA, Sauer JM. Truong AP, et al. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6231-6. doi: 10.1016/j.bmcl.2010.08.102. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20833041
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.
Semko CM, Chen L, Dressen DB, Dreyer ML, Dunn W, Farouz FS, Freedman SB, Holsztynska EJ, Jefferies M, Konradi AW, Liao A, Lugar J, Mutter L, Pleiss MA, Quinn KP, Thompson T, Thorsett ED, Vandevert C, Xu YZ, Yednock TA. Semko CM, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1741-3. doi: 10.1016/j.bmcl.2011.01.075. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316228
Orally available and efficacious α4β1/α4β7 integrin inhibitors.
Xu YZ, Smith JL, Semko CM, Rossiter KI, Fukuda JY, Dappen MS, Quincy DA, Konradi AW, Mao W, Welch B, Dreyer ML, Samant B, Zhang H, Lugar J, Liao Z, Henschel C, Petersen E, Vandevert C, Shoemaker M, Wehner N, Mutter L, Shopp G, Krimm M, Chen L, Wipke B, Dofiles L, Gallager I, Sauer JM, Messersmith EK, Pleiss MA, Bard F, Yednock TA. Xu YZ, et al. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4370-3. doi: 10.1016/j.bmcl.2013.05.076. Epub 2013 May 31. Bioorg Med Chem Lett. 2013. PMID: 23777782
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958.
Hawkinson JE, Szoke BG, Garofalo AW, Hom DS, Zhang H, Dreyer M, Fukuda JY, Chen L, Samant B, Simmonds S, Zeitz KP, Wadsworth A, Liao A, Chavez RA, Zmolek W, Ruslim L, Bova MP, Holcomb R, Butelman ER, Ko MC, Malmberg AB. Hawkinson JE, et al. J Pharmacol Exp Ther. 2007 Aug;322(2):619-30. doi: 10.1124/jpet.107.120352. Epub 2007 Apr 30. J Pharmacol Exp Ther. 2007. PMID: 17470643
450 results